HK2-IN-3
HK2-IN-3 is a selective HK2 inhibitor with a human IC50 of 0.0564 μM (56.4 nM). HK2-IN-3 induces mitophagy in oral squamous cell carcinoma cells. HK2-IN-3 exerts anti-cancer activity in oral squamous cell carcinoma cells. HK2-IN-3 can be used for the research of oral squamous cell carcinoma.
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- CAS No.: 2679261-30-2
- 화학식: C15H11N3O4S
- 분자량:329.33
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
IC50 & Target
[1]|
HK2 56.4 nM (IC50) |
GLUT1 |
GLUT4 |
In Vitro
HK2-IN-3 (100 ns) binds selectively and stably to HK2 over HK1, with binding energies ranging between -190 and -270 kcal/mol and persistent interactions with critical HK2 active site residues[1].
HK2-IN-3 (1-5 μM; 72 h) reduces glucose uptake in Cal27 and FaDu OSCC cells when treated at 1, 3, or 5 μM for 72 h[1].
HK2-IN-3 (5 μM) disrupts the 3D structure of Cal27 OSCC spheroids and increases cell death when treated at 5 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Cal27 OSCC cells
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Concentration:10 μM; 30 μM
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Incubation Time:4 h
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Result:At 10 and 30 μM, induced dose-dependent dissociation of mitochondrial HK2 (mitoHK2) to the cytosol without altering total intracellular HK2 levels.
At 30 μM, significantly increased LC3-I and LC3-II levels in both mitochondrial and cytosolic fractions, and decreased p62 levels in mitochondrial fractions; immunofluorescence showed increased LC3B puncta formation and colocalization with mitochondria, confirming mitophagy induction.
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Cell Line:Cal27 OSCC cells
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Concentration:3 μM; 10 μM; 30 μM
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Incubation Time:72 h
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Result:At 10 μM, reduced GLUT1 expression; at 30 μM, significantly downregulated expression of GLUT1, GLUT4, EGFR, and VEGF.
Lower concentrations (3 μM) did not alter GLUT1 or GLUT4 expression despite reducing glucose uptake.
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Cell Line:Cal27 OSCC cells
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Concentration:5 μM
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Incubation Time:72 h
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Result:Induced early to late apoptosis in Cal27 cells, with higher apoptosis-inducing activity than compound 13 at the same concentration.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:immunocompromised mice (5-week-old)[1]
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Dosage:3 mg/kg; 10 mg/kg
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Administration:i.p.; daily; 16 days
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Result:Induced a significant, dose-dependent reduction in tumor volumes over the 16-day treatment period, with no notable decrease in animal body weight.
Observed a dose-dependent reduction in tumor weights.
Significantly down-regulated GLUT1, EGFR, and VEGF gene expression in tumor tissues at both 3 mg/kg and 10 mg/kg.
Significantly down-regulated mesenchymal marker N-cadherin gene expression in tumor tissues.
Showed a dose-dependent dissociation of mitochondrial HK2, a decrease in p62 levels, and an increase in LC3II levels in mitochondrial fractions from tumor tissues, indicating induction of mitophagy.
Showed no changes in total HK2 levels in total tumor lysates.
Reduced invasion to the dermal region and caused degenerative alterations in tumor tissues compared to the disease control group.
Chemical Information
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CAS No. 2679261-30-2
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분자량 329.33
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화학식 C15H11N3O4S
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SMILES
O=C(N/N=C/C1=C(O)C(O)=C(O)C=C1)C(S2)=NC3=C2C=CC=C3
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Hot Topics
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Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HK2-IN-3 Related Classifications
HY-180805 Related Classifications
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